Clinical and pharmacological group: & nbsp

ACE Inhibitors

Included in the formulation
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  • Hopten®
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  • АТХ:

    C.09.A.A.10   Trandolapril

    Pharmacodynamics:

    Strongly binds to the ACE. Inhibition of ACE leads to a decrease in angiotensin concentration II, aldosterone, atrial natriuretic factor, increased plasma renin activity and angiotensin concentration I. In this way, trandolapril modulates the renin-angiotensin-aldosterone system, which plays a major role in regulating the volume of circulating blood and blood pressure, and consistently exerts an antihypertensive effect.

    Pharmacokinetics:

    Time to reach the maximum concentration in the blood plasma - about 1 hour. Communication with blood plasma proteins - 80%. Metabolised in the liver with the formation of an active metabolite - trandolaprilata. Effective half-life is 16-24 hours, and the terminal half-life varies from 47 to 98 hours depending on the dose.

    Indications:

    Essential arterial hypertension.

    Heart failure (secondary prophylaxis after myocardial infarction with a decrease in the left ventricular ejection fraction on day 3 after its development).

    IX.I10-I15.I10   Essential [primary] hypertension

    IX.I30-I52.I50.0   Congestive heart failure

    Contraindications:
    • Angioedema, including those noted with prior treatment with ACE inhibitors.
    • Hereditary or idiopathic angioedema.
    • Aortic stenosis or obstruction of the outflow tract of the left ventricle.
    • Pregnancy.
    • Lactation period (breastfeeding).
    • Children and adolescence under 18 years.
    • Hypersensitivity to the drug.
    Carefully:Hypersensitivity.
    Pregnancy and lactation:

    The drug is contraindicated for use in pregnancy and lactation (breastfeeding).

    Category of recommendations for FDA is not defined.

    Dosing and Administration:Arterial hypertension - 2-8 mg per day. The maximum daily dose is 2 mg.

    Cardiac insufficiency (secondary prophylaxis after myocardial infarction begins on the third day after its development, after the reduction of the left ventricular ejection fraction) - 2-4 mg. The maximum daily dose is 16 mg.

    For patients with impaired renal function or moderate impairment of liver function, with violations of the water-electrolyte balance, the initial dose is 0.5 mg once a day.In severe violations of the liver and kidneys (creatinine clearance less than 30 ml / min) should reduce the dose.

    Side effects:

    On the part of the system hematopoiesis: agranulocytosis, leukopenia, pancytopenia.

    Allergic reactions: reactions of hypersensitivity, including pruritus and rash, angioedema.

    From the side respiratory system: dyspnea, bronchitis.

    From the side digestive system: nausea, vomiting, abdominal pain, diarrhea, dry mouth, increased activity of hepatic enzymes (including ACT and ALT).

    Dermatological reactions: alopecia, increased sweating.

    From the side urinary system: increase in residual urea nitrogen and serum creatinine.

    Other: fever.

    The following are undesirable events that were recorded with all ACE inhibitors:

    From the side hematopoiesis system: pancytopenia.

    From the side CNS: transient ischemic attacks, stroke.

    From the side of cardio-vascular system: stenocardia, myocardial infarction, atrioventricular blockade, bradycardia, cardiac arrest, tachycardia.

    From the side digestive system: pancreatitis.

    Dermatological reactions: erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

    From the side musculoskeletal system: myalgia.

    From the side laboratory research: decrease in hemoglobin, decrease in hematocrit.

    Overdose:

    Possible symptoms: marked decrease in blood pressure, shock, stupor, bradycardia, electrolyte disorders, renal failure.

    Treatment symptomatic.

    Interaction:

    Diuretics or other antihypertensives with simultaneous use can enhance the antihypertensive effect of trandolapril. Adrenoblockers should be used in combination with trandolapril only after careful observation.

    With the simultaneous use of trandolapril with potassium preparations, potassium-sparing diuretics (spironolactone, amiloride, triamterene) there is a significant increase in potassium concentration in the blood serum, especially in cases of impaired renal function. Trandolapril can reduce potassium loss with the use of thiazide diuretics.

    The simultaneous use of trandolapril with hypoglycemic drugs (insulin or oral hypoglycemic drugs) can enhance the effect of the latter and lead to an increased risk of hypoglycemia.

    With the simultaneous use of trandolapril with lithium preparations, the concentration of lithium in the blood serum increases due to the deterioration of its excretion.

    With the simultaneous use of trandolapril with funds for inhalation anesthesia, there is an increase in hypotensive effect.

    With the simultaneous use of trandolapril with cytostatics, systemic glucocorticosteroids and immunosuppressive drugs, the risk of developing leukopenia increases.

    Clinically significant signs of the interaction of trandolapril with thrombolytics, acetylsalicylic acid, beta-adrenoblockers, calcium channel blockers, nitrates, anticoagulants or digoxin in patients with left ventricular failure after myocardial infarction were not noted.

    Special instructions:

    Trandolapril is a prodrug that turns into an active form in the liver, so special care must be taken in patients with impaired function.

    In patients with uncomplicated arterial hypertension after the first dose of trandolapril, and also after its increase, the development of arterial hypotension accompanied by clinical symptoms was noted.The risk of developing hypotension is higher in patients who have a deficiency of fluid and salt, resulting from prolonged diuretic therapy, limiting salt intake, dialysis, diarrhea, or vomiting. In such patients, before starting therapy with trandolapril, diuretic therapy should be discontinued and the volume of circulating blood and / or salt content should be replenished.

    In the treatment of ACE inhibitors, cases of agranulocytosis and bone marrow suppression have been described. These undesirable phenomena are more common in disorders of kidney function, especially in patients with diffuse connective tissue diseases. In such patients (for example, in systemic lupus erythematosus or systemic scleroderma), it is advisable to regularly monitor the number of leukocytes in the blood and the protein content in the urine, especially if the kidney function is impaired and treated with glucocorticosteroids and antimetabolites.

    The use of trandolapril can cause angioedema, swelling of the face, limbs, tongue, throat and / or larynx.

    In some patients receiving diuretics (especially recently), after the appointment of trandolapril, a sharp drop in blood pressure is observed.

    In case of severe renal insufficiency, a dose reduction of trandolapril may be required; kidney function should be carefully monitored.

    In patients with renal insufficiency, chronic heart failure, bilateral stenosis of the renal arteries or unilateral stenosis of the artery of a single functioning kidney, the risk of worsening kidney function is increased. In some patients, arterial hypertension without kidney disease with the appointment of trandolapril in combination with a diuretic may increase blood urea nitrogen and serum creatinine levels. Proteinuria may occur.

    In patients with arterial hypertension with concomitant renal dysfunction with the use of trandolapril, hyperkalemia may occur.

    With surgical interventions or general anesthesia using drugs that cause arterial hypotension, trandolapril can block the secondary formation of angiotensin II associated with compensatory release of renin.

    When using high-permeable polyacrylonitrile membranes during hemodialysis in patients receiving ACE inhibitors, anaphylactoid reactions were described.The use of such membranes should be avoided in the administration of ACE inhibitors to patients on hemodialysis.

    The safety and effectiveness of the use of trandolapril in children has not been studied, so its use in children is not recommended.

    Impact on the ability to drive vehicles and manage mechanisms.

    Based on the pharmacological properties of trandolapril, the ability to drive vehicles or work with complex equipment should not change. However, in some patients with simultaneous intake of alcoholic beverages, especially at the initial stages of treatment with ACE inhibitors or when replacing one drug with another, an increase in the level of ethanol in the blood can be observed and its elimination can be slowed down. As a result, the effects of alcohol can increase. Therefore, with simultaneous reception with alcohol, after the first intake or with a significant increase in the dose of trandolapril for several hours, it is not recommended to drive vehicles or work with mechanisms.

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